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Prodrugs of a 1'-CN-4-Aza-7,9-dideazaadenosine C-Nucleoside Leading to the Discovery of Remdesivir (GS-5734) as a Potent Inhibitor of Respiratory Syncytial Virus with Efficacy in the African Green Monkey Model of RSV.
Mackman RL, Hui HC, Perron M, Murakami E, Palmiotti C, Lee G, Stray K, Zhang L, Goyal B, Chun K, Byun D, Siegel D, Simonovich S, Du Pont V, Pitts J, Babusis D, Vijjapurapu A, Lu X, Kim C, Zhao X, Chan J, Ma B, Lye D, Vandersteen A, Wortman S, Barrett KT, Toteva M, Jordan R, Subramanian R, Bilello JP, Cihlar T. Mackman RL, et al. Among authors: lee g. J Med Chem. 2021 Apr 22;64(8):5001-5017. doi: 10.1021/acs.jmedchem.1c00071. Epub 2021 Apr 9. J Med Chem. 2021. PMID: 33835812
Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit.
Brown ML, Aaron W, Austin RJ, Chong A, Huang T, Jiang B, Kaizerman JA, Lee G, Lucas BS, McMinn DL, Orf J, Rong M, Toteva MM, Xu G, Ye Q, Zhong W, Degraffenreid MR, Wickramasinghe D, Powers JP, Hungate R, Johnson MG. Brown ML, et al. Among authors: lee g. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5206-9. doi: 10.1016/j.bmcl.2011.07.052. Epub 2011 Jul 23. Bioorg Med Chem Lett. 2011. PMID: 21840217
Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study.
Mackman RL, Sangi M, Sperandio D, Parrish JP, Eisenberg E, Perron M, Hui H, Zhang L, Siegel D, Yang H, Saunders O, Boojamra C, Lee G, Samuel D, Babaoglu K, Carey A, Gilbert BE, Piedra PA, Strickley R, Iwata Q, Hayes J, Stray K, Kinkade A, Theodore D, Jordan R, Desai M, Cihlar T. Mackman RL, et al. Among authors: lee g. J Med Chem. 2015 Feb 26;58(4):1630-43. doi: 10.1021/jm5017768. Epub 2015 Jan 27. J Med Chem. 2015. PMID: 25574686 Clinical Trial.
Highly Selective Phosphatidylinositol 4-Kinase IIIβ Inhibitors and Structural Insight into Their Mode of Action.
Mejdrová I, Chalupská D, Kögler M, Šála M, Plačková P, Baumlová A, Hřebabecký H, Procházková E, Dejmek M, Guillon R, Strunin D, Weber J, Lee G, Birkus G, Mertlíková-Kaiserová H, Boura E, Nencka R. Mejdrová I, et al. Among authors: lee g. J Med Chem. 2015 May 14;58(9):3767-93. doi: 10.1021/acs.jmedchem.5b00499. Epub 2015 May 4. J Med Chem. 2015. PMID: 25897704
Discovery of β-D-2'-deoxy-2'-α-fluoro-4'-α-cyano-5-aza-7,9-dideaza adenosine as a potent nucleoside inhibitor of respiratory syncytial virus with excellent selectivity over mitochondrial RNA and DNA polymerases.
Clarke MO, Mackman R, Byun D, Hui H, Barauskas O, Birkus G, Chun BK, Doerffler E, Feng J, Karki K, Lee G, Perron M, Siegel D, Swaminathan S, Lee W. Clarke MO, et al. Among authors: lee g, lee w. Bioorg Med Chem Lett. 2015 Jun 15;25(12):2484-7. doi: 10.1016/j.bmcl.2015.04.073. Epub 2015 Apr 29. Bioorg Med Chem Lett. 2015. PMID: 25978965
Purine analogs as phosphatidylinositol 4-kinase IIIβ inhibitors.
Šála M, Kögler M, Plačková P, Mejdrová I, Hřebabecký H, Procházková E, Strunin D, Lee G, Birkus G, Weber J, Mertlíková-Kaiserová H, Nencka R. Šála M, et al. Among authors: lee g. Bioorg Med Chem Lett. 2016 Jun 1;26(11):2706-12. doi: 10.1016/j.bmcl.2016.04.002. Epub 2016 Apr 5. Bioorg Med Chem Lett. 2016. PMID: 27090557 Free PMC article.
Rational Design of Novel Highly Potent and Selective Phosphatidylinositol 4-Kinase IIIβ (PI4KB) Inhibitors as Broad-Spectrum Antiviral Agents and Tools for Chemical Biology.
Mejdrová I, Chalupská D, Plačková P, Müller C, Šála M, Klíma M, Baumlová A, Hřebabecký H, Procházková E, Dejmek M, Strunin D, Weber J, Lee G, Matoušová M, Mertlíková-Kaiserová H, Ziebuhr J, Birkus G, Boura E, Nencka R. Mejdrová I, et al. Among authors: lee g. J Med Chem. 2017 Jan 12;60(1):100-118. doi: 10.1021/acs.jmedchem.6b01465. Epub 2016 Dec 22. J Med Chem. 2017. PMID: 28004945
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.
Siegel D, Hui HC, Doerffler E, Clarke MO, Chun K, Zhang L, Neville S, Carra E, Lew W, Ross B, Wang Q, Wolfe L, Jordan R, Soloveva V, Knox J, Perry J, Perron M, Stray KM, Barauskas O, Feng JY, Xu Y, Lee G, Rheingold AL, Ray AS, Bannister R, Strickley R, Swaminathan S, Lee WA, Bavari S, Cihlar T, Lo MK, Warren TK, Mackman RL. Siegel D, et al. Among authors: lee g, lee wa. J Med Chem. 2017 Mar 9;60(5):1648-1661. doi: 10.1021/acs.jmedchem.6b01594. Epub 2017 Feb 14. J Med Chem. 2017. PMID: 28124907
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